Structure–Activity Relationship of Phytoestrogen Analogs as ERα/β Agonists with Neuroprotective Activities
نویسندگان
چکیده
A set of isoflavononid and flavonoid analogs was prepared evaluated for estrogen receptor α (ERα) ERβ transactivation anti-neuroinflammatory activities. Structure–activity relationship (SAR) study naturally occurring phytoestrogens, their metabolites, related isoflavone revealed the importance C-ring isoflavonoids ER activity selectivity. Docking suggested putative binding modes daidzein 2 dehydroequol 8 in active site ERα ERβ, provided an understanding promising selectivity 8. Among tested compounds, equol 7 were most potent ERα/β agonists with neuroprotective activity. This provides knowledge on SAR further development selective potential.
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ژورنال
عنوان ژورنال: Chemical & Pharmaceutical Bulletin
سال: 2021
ISSN: ['0009-2363', '1347-5223']
DOI: https://doi.org/10.1248/cpb.c20-00706